Novel compounds having a tetracyclic iridoid skelton and an anti-trypanosomal agent comprising the same as an active ingredient

Abstract

The present invention provides anti-trypanosomal agent for treating, preventing Trypanosomiasis of mammals, which comprises a compound having the tetracyclic iridoid skeleton represented by a general formula (I).

1 . A compound having the tetracyclic iridoid skeleton represented by a general formula (I). 
       
         
           
           
               
               
           
         
       
       wherein R 1  and R 2  are independently, hydrogen or C 1 -C 8  alkyl. 
     
     
         2 . The compound according to  claim 1 , which is isolated from  Morinda lucida.   
     
     
         3 . The compound according to  claim 1 , which is represented by a formula (II). 
       
         
           
           
               
               
           
         
       
     
     
         4 . The compound according to  claim 1 , which is represented by a formula (III). 
       
         
           
           
               
               
           
         
       
     
     
         5 . An anti-trypanosomal agent for preventing or treating Trypanosomiasis comprising the compound according to  claim 1  as an active ingredient. 
     
     
         6 . The anti-trypanosomal agent according to  claim 5 , which comprises the compound according to  claim 3  as an active ingredient. 
     
     
         7 . The anti-trypanosomal agent according to  claim 5 , which comprises the compound according to  claim 4  as an active ingredient. 
     
     
         8 . The anti-trypanosomal agent according to  claim 5 , wherein the Trypanosomiasis is African Trypanosomiasis or American Trypanosomiasis. 
     
     
         9 . The anti-trypanosomal agent according to  claim 5 , which has low cytotoxicity on mammalian cells. 
     
     
         10 . The anti-trypanosomal agent according to  claim 5 , wherein the selectivity index (SI) of the compound on normal human fibroblast is more than 8. 
     
     
         11 . A method for preventing or treating Trypanosomiasis, which comprises administering the compound according to  claim 1  to a mammal. 
     
     
         12 . The method for preventing or treating Trypanosomiasis according to  claim 11 , which comprises administering the compound according to  claim 3  to a mammal. 
     
     
         13 . The method for preventing or treating Trypanosomiasis according to  claim 11 , which comprises administering the compound according to  claim 4  to a mammal. 
     
     
         14 . The method according to  claim 11 , wherein the Trypanosomiasis is African Trypanosomiasis or American Trypanosomiasis. 
     
     
         15 . The method according to  claim 11 , wherein the compound has low cytotoxicity on mammalian cells. 
     
     
         16 . The method according to  claim 11 , wherein the selectivity index (SI) of the compound on normal human fibroblast is more than 8. 
     
     
         17 . The method according to  claim 11 , wherein the subject is a domestic animal. 
     
     
         18 . The method according to  claim 11 , wherein the subject is a human.